申请人:IMPERIAL CHEMICAL INDUSTRIES PLC
公开号:EP0125091A2
公开(公告)日:1984-11-14
A4,4'-alkylenebis[piperidine-1-(N-amidino-amidine)] derivative of the formula:-
or a tautomeric form thereof, wherein each ofR1,R2, R' and R4, which may be the same or different, is hydrogen or an alkyl, alkenyl or alkoxyalkyl radical of up to 20 carbon atoms; or R', R2 and the nitrogen atom to which they are attached, or R' and R4 and the nitrogen atom to which they are attached, which may be the same or different, are each a 1-azetidinyl, 1-pyrrolidinyl, piperidino, hexamethyleneimino, heptamethyleneimino, morpholino or 4-(1-8C alkanoyl)-1-piperazinyl radical each of which may bear 1-3C alkyl substituents; a 3-20C cycloalkyl radical; or an optionally substituted phenyl or phenylalkyl radical; provided that at least one ofR', R', R' and R4 is otherthan hydrogen; X is a direct bond or a 1-6C straight- or branched-chain alkylene radical which is linked to the 3- or 4-positions of the piperidine rings; and R5 and R5, which may be the same or different, are each hydrogen or a 1-8C alkyl radical; and the acid addition salts thereof, processes for their manufacture, and antibacterial and antifungal compositions and methods using said compounds.
A4,4'-亚烷基双[
哌啶-1-(N-脒基-脒)]衍
生物,其式如下
或其同分异构体形式,其中 R1、R2、R'和 R4(可以相同或不同)各自为氢或碳原子数不超过 20 个的烷基、烯基或烷氧基烷基;或 R'、R2 及其所连接的氮原子,或 R'、R4 及其所连接的氮原子(可以相同或不同)各自为 1-氮杂
环丁基、1-
吡咯烷基、
哌啶基、六亚甲基亚
氨基、七亚甲基亚
氨基、吗啉基或 4-(1-8C烷酰基)-1-
哌嗪基,其中每个基团可带有 1-3C 烷基取代基;3-20C环烷基;或任选取代的苯基或苯基烷基;条件是 R'、R'、R'和 R4 中至少有一个不是氢;X 是直接键或 1-6C 直链或支链亚烷基,与
哌啶环的 3 位或 4 位相连;以及 R5 和 R5(可以相同或不同)各自为氢或 1-8C 烷基;及其酸加成盐、其制造工艺以及使用所述化合物的抗菌和抗真菌组合物和方法。